Yang Dan-Dan, Chutiwitoonchai Nopporn, Wang Feng, Tian Ping, Sureram Sanya, Lei Xiaoguang, Mahidol Chulabhorn, Ruchirawat Somsak, Kittakoop Prasat
Chulabhorn Graduate Institute, Program in Chemical Sciences, Laksi, Bangkok, 10210, Thailand.
Virology and Cell Technology Research Team, National Center for Genetic Engineering and Biotechnology (BIOTEC), National Science and Technology Development Agency (NSTDA), 113 Thailand Science Park, Phahonyothin Rd, Pathumthani, 12120, Thailand.
Sci Rep. 2025 Feb 21;15(1):6380. doi: 10.1038/s41598-025-89736-0.
The present work investigates virucidal and antiviral compounds in the extracts of seed embryos of a lotus, Nelumbo nucifera, and a Thai ginseng, Kaempferia parviflora. Separation of the extracts led to the identification of antiviral compounds against SARS-CoV-2. Neferine (1) and nuciferine (3) from N. nucifera, as well as their respective HCl salts (2 and 4), exhibited virucidal and antiviral activities against SARS-CoV-2. Virucidal activity of neferine salt (2) (EC 4.78 µM) was 7.5 times better than its free-base, neferine (1) (EC 36.01 µM), and the salt (2) also improved the selectivity index (SI), showing less cytotoxicity than 1. This work demonstrates that organic salts have an impact on biological activities. A crude extract of K. parviflora rhizomes displayed virucidal activity (EC 42.11 µg/mL) and antiviral activity (EC 39.28 µg/mL). Isolation of a crude extract of K. parviflora rhizomes led to the identification of nine flavonoids (5-13). Among these flavonoids, only 5,7,4'-trimethoxyflavone (8) was found to show virucidal (EC 437.90 µM) and antiviral (EC 50.97 µM) activities against SARS-CoV-2. However, flavonoids (5-13) did not inhibit SARS-CoV-2 3CL enzyme at the concentrations of 10 µM and 100 µM. In conclusion, our data underscores the therapeutic potential of N. nucifera and K. parviflora derived bioactive compounds against SARS-CoV-2.
本研究调查了莲花(Nelumbo nucifera)种子胚提取物和泰国人参(Kaempferia parviflora)中的杀病毒和抗病毒化合物。提取物的分离导致鉴定出针对严重急性呼吸综合征冠状病毒2(SARS-CoV-2)的抗病毒化合物。莲心碱(1)和荷叶碱(3)以及它们各自的盐酸盐(2和4)对SARS-CoV-2表现出杀病毒和抗病毒活性。莲心碱盐(2)(半数有效浓度[EC]为4.78 μM)的杀病毒活性比其游离碱莲心碱(1)(EC为36.01 μM)高7.5倍,并且盐(2)还提高了选择性指数(SI),显示出比1更低的细胞毒性。这项工作表明有机盐对生物活性有影响。小花山柰根茎的粗提物显示出杀病毒活性(EC为42.11 μg/mL)和抗病毒活性(EC为39.28 μg/mL)。小花山柰根茎粗提物的分离导致鉴定出九种黄酮类化合物(5 - 13)。在这些黄酮类化合物中,仅发现5,7,4'-三甲氧基黄酮(8)对SARS-CoV-2表现出杀病毒(EC为437.90 μM)和抗病毒(EC为50.97 μM)活性。然而,黄酮类化合物(5 - 13)在10 μM和100 μM浓度下未抑制SARS-CoV-2 3C样蛋白酶。总之,我们的数据强调了莲和小花山柰衍生的生物活性化合物对SARS-CoV-2的治疗潜力。